CECXG explained

CECXG (3'-ethyl-LY-341,495) is a research drug which acts as a potent and selective antagonist for the group II metabotropic glutamate receptors (mGluR2/3), with reasonable selectivity for mGluR3. While it is some five times less potent than LY-341,495 at mGluR3, it has 38x higher affinity for mGluR3 over mGluR2,[1] making it one of the few ligands available that is able to distinguish between these two closely related receptor subtypes.[2] [3] [4]

Notes and References

  1. Collado I, Ezquerra J, Mazón A, Pedregal C, Yruretagoyena B, Kingston AE, Tomlinson R, Wright RA, Johnson BG, Schoepp DD . 6 . 2,3'-disubstituted-2-(2'-carboxycyclopropyl)glycines as potent and selective antagonists of metabotropic glutamate receptors . Bioorganic & Medicinal Chemistry Letters . 8 . 20 . 2849–2854 . October 1998 . 9873635 . 10.1016/S0960-894X(98)00510-1 .
  2. Book: Schoepp DD, Jane DE, Monn JA . Pharmacology of metabotropic glutamate receptors . Egebjerg J, Krogsgaard-Larsen P, Schousboe A . Glutamate and GABA receptors and transporters: structure, function and pharmacology . 171–173 . Taylor & Francis . 2002 . 0-7484-0881-9 .
  3. Sørensen US, Bleisch TJ, Kingston AE, Wright RA, Johnson BG, Schoepp DD, Ornstein PL . Synthesis and structure-activity relationship studies of novel 2-diarylethyl substituted (2-carboxycycloprop-1-yl)glycines as high-affinity group II metabotropic glutamate receptor ligands . Bioorganic & Medicinal Chemistry . 11 . 2 . 197–205 . January 2003 . 12470714 . 10.1016/S0968-0896(02)00387-5 .
  4. Ure J, Baudry M, Perassolo M . Metabotropic glutamate receptors and epilepsy . Journal of the Neurological Sciences . 247 . 1 . 1–9 . August 2006 . 16697014 . 10.1016/j.jns.2006.03.018 . 22777207 .

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